Category: 1193-21-1

In 2019,Journal of Medicinal Chemistry included an article by Liang, Xiaofei; Wang, Beilei; Chen, Cheng; Wang, Aoli; Hu, Chen; Zou, Fengming; Yu, Kailin; Liu, Qingwang; Li, Feng; Hu, Zhenquan; Lu, Tingting; Wang, Junjie; Wang, Li; Weisberg, Ellen L.; Li, Lili; Xia, Ruixiang; Wang, Wenchao; Ren, Tao; Ge, Jian; Liu, Jing; Liu, Qingsong. Related Products of 1193-21-1. The article was titled 《Discovery of N-(4-(6-acetamidopyrimidin-4-yloxy)phenyl)-2-(2-(trifluoromethyl)phenyl)acetamide (CHMFL-FLT3-335) as a potent FMS-like tyrosine kinase 3 internal tandem duplication (FLT3-ITD) mutant selective inhibitor for acute myeloid leukemia》. The information in the text is summarized as follows:

Most of the current FMS-like tyrosine kinase 3 (FLT3) inhibitors lack selectivity between FLT3 kinase and cKIT kinase as well as the FLT3 wt and internal tandem duplication (ITD) mutants. We report a new compound I, which displays GI50 values of 30-80 nM against different ITD mutants and achieves selectivity over both FLT3 wt (8-fold) and cKIT kinase in the transformed BaF3 cells (>300-fold). I potently inhibits the proliferation of the FLT3-ITD-pos. acute myeloid leukemia cancer lines through suppression of the phosphorylation of FLT3 kinase and downstream signaling pathways, induction of apoptosis, and arresting the cell cycle into the G0/G1 phase. I also displays potent antiproliferative effect against FLT3-ITD-pos. patient primary cells, whereas it does not apparently affect FLT3 wt primary cells. In addition, it also exhibits a good therapeutic window to PBMC compared to PKC412. In the in vivo studies, I demonstrates favorable PK profiles and suppresses the tumor growth in the MV4-11 cell inoculated mouse xenograft model. In the experimental materials used by the author, we found 4,6-Dichloropyrimidine(cas: 1193-21-1Related Products of 1193-21-1)

4,6-Dichloropyrimidine(cas: 1193-21-1) is a member of organic chlorides. Almost all organochlorine compounds are synthesized. It is widely used as intermediates, solvents and pesticides of chemical synthetic products.Related Products of 1193-21-1

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

《Tyrosine kinase inhibitor prodrug-loaded liposomes for controlled release at tumor microenvironment》 was written by Salmaso, Stefano; Mastrotto, Francesca; Roverso, Marco; Gandin, Valentina; De Martin, Sara; Gabbia, Daniela; De Franco, Michele; Vaccarin, Christian; Verona, Marco; Chilin, Adriana; Caliceti, Paolo; Bogialli, Sara; Marzaro, Giovanni. HPLC of Formula: 1193-21-1This research focused ontyrosine kinase inhibitor prodrug liposomes controlled release tumor microenvironment; Drug release; Kinase inhibitors; Liposomes; Microsomes; pH-dependent hydrolysis. The article conveys some information:

Tyrosine kinase inhibitors (TKIs) represent one of the most advanced class of therapeutics for cancer treatment. Most of them are also cytochrome P 450 (CYP) inhibitors and/or substrates thereof. Accordingly, their efficacy and/or toxicity can be affected by CYP-mediated metabolism and by metabolism-derived drug-drug interactions. In order to enhance the therapeutic performance of these drugs, we developed a prodrug (Pro962) of our TKI TK962 specifically designed for liposome loading and pH-controlled release in the tumor. A cholesterol moiety was linked to TK962 through pH-sensitive hydrazone bond for anchoring to the liposome phospholipid bilayer to prevent leakage of the prodrug from the nanocarrier. Bioactivity studies performed on isolated target kinases showed that the prodrug maintains only partial activity against them and the release of TK962 is required. Biopharmaceutical studies carried out with prodrug loaded liposomes showed that the prodrug was firmly associated with the vesicles and the drug release was prevented under blood-mimicking conditions. Conversely, conventional liposome loaded with TK962 readily released the drug. Flow cytometric studies showed that liposomes efficiently provided for intracellular prodrug delivery. The use of the hydrazone linker yielded a pH-controlled drug release, which resulted in about 50% drug release at pH 4 and 5 in 2 h. Prodrug, prodrug loaded liposomes and active lead compound have been tested against cancer cell lines in either 2D or 3D models. The liposome formulation showed higher cytotoxicity than the unformulated lead TK962 in both 2D and 3D models. The stability of prodrug, prodrug loaded liposomes and active lead compound in human serum and against human, mouse, and rat microsomes was also assessed, demonstrating that liposome formulations impair the metabolic reactions and protect the loaded compounds from catabolism. The results suggest that the liposomal formulation of pH releasable TKI prodrugs is a promising strategy to improve the metabolic stability, intracellular cancer cell delivery and release, and in turn the efficacy of this class of anticancer drugs. In the experiment, the researchers used 4,6-Dichloropyrimidine(cas: 1193-21-1HPLC of Formula: 1193-21-1)

4,6-Dichloropyrimidine(cas: 1193-21-1) is a member of organic chlorides. Organic chlorides are compounds containing a carbon-chlorine bond, which are widely used in the oil field as a wax dissolver. They are generally not present in crude oils and are typically the result of additives, cleaning solutions or chemicals used for oil recovery.HPLC of Formula: 1193-21-1

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 2022,Ayala, Caitlan E.; Perez, Rocio L.; Mathaga, John K.; Watson, Aanesa; Evans, Tristan; Warner, Isiah M. published an article in ACS Applied Polymer Materials. The title of the article was 《Fluorescent Ionic Probe for Determination of Mechanical Properties of Healed Poly(ethylene-co-methacrylic acid) Ionomer Films》.Product Details of 1193-21-1 The author mentioned the following in the article:

In recent years, advanced materials with properties resembling biol. systems, particularly artificial muscles, have received intense scrutiny. This is because the interesting conformational shape characteristics of such materials have benefited a variety of technologies, including textiles, 3D printing, and medical devices. Although a multitude of shape memory properties have been studied and developed in recent years, self-healing of these polymers after puncture or rupture has also become a major area of study. Most techniques for detection of such processes are mech. based and require considerable hands-on monitoring. Thus, a rapid visual detection method for self-healing is highly desirable. Herein, we describe fluorescence studies for rapid detection of self-healing properties of a partially neutralized sodium ionomer poly(ethylene-co-methacrylic acid) (PEMA). In this study, two different fluorophores, parent non-ionic 4,6-dipyrenylpyrimidine and ionic 4,6-dipyrenylpyrimidinium iodide fluorophores, were evaluated as possible sensors of self-healing. Incorporation of these probes via solution blending and compatibility into a PEMA of these fluorophores were evaluated. Thermal characterizations using differential scanning calorimetry were also performed to elucidate phys. characteristics of healed sites. Ratiometric fluorescence emission variations were explored within puncture-healed ionomer films and related to Young’s modulus properties with good linearity, indicating potential utility of this approach for monitoring elastic modulus properties after healing has occurred. Further statistical analyses of mech. processes using quadratic discriminant anal. resulted in development of several highly accurate predictive models for determining time since damage healing. In the experiment, the researchers used many compounds, for example, 4,6-Dichloropyrimidine(cas: 1193-21-1Product Details of 1193-21-1)

4,6-Dichloropyrimidine(cas: 1193-21-1) is a member of organic chlorides. Organic chloride content in crude oil can be detected through specialized laboratory analysis. Care and attention are essential while sampling and testing.Product Details of 1193-21-1

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 2022,Vavaiya, Bhavinkumar; Patel, Shivani; Pansuriya, Vrajlal; Marvaniya, Vanita; Patel, Popatbhai published an article in Asian Journal of Chemistry. The title of the article was 《In silico and in vitro antitubercular studies for nitrogen rich hybrids of homopiperazine-pyrimidine-pyrazole adducts》.Computed Properties of C4H2Cl2N2 The author mentioned the following in the article:

Novel homopiperazine-pyrimidine-pyrazole hybrids (3a-j) were synthesized using Et 2-cyanoacetate and 4,6-dichloropyrimidine as starting materials by a multi-step process to afford Et 5-amino-1-(6-chloropyrimidin-4-yl)-1H-pyrazole-4-carboxylate in good yields using polar protic media. The intermediate 1, in two steps, chloroamine condensation followed by acid amine coupling, furnished the title compounds Et 5-amino-1-(6-(4-substituted aryl-1,4-diazepan-1-yl)pyrimidin-4-yl)-1H-pyrazole-4-carboxylate (3a-j). The synthesized compounds were docked in the crystal structure of Mycobacterium tuberculosis (PDB ID: 4TRO) to get insights into structural requirements for antitubercular activity. In vitro antitubercular activity against M. tuberculosis H37Rv strains showed that compounds 3a, 3d, 3e and 3g were found to be the most potent (Docking score: > -21; MIC = 1.6 μg/mL) among the synthesized mols. All the synthesized compounds showed acceptable drug-like properties which make them suitable for further lead modification using in silico design approaches. In the part of experimental materials, we found many familiar compounds, such as 4,6-Dichloropyrimidine(cas: 1193-21-1Computed Properties of C4H2Cl2N2)

4,6-Dichloropyrimidine(cas: 1193-21-1) is a member of organic chlorides. Organic chloride content in crude oil can be detected through specialized laboratory analysis. Care and attention are essential while sampling and testing.Computed Properties of C4H2Cl2N2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 2022,Bhuyan, Amar Jyoti; Bharali, Sourav Jyoti; Sharma, Abhilash; Dutta, Dhiraj; Gogoi, Pranjal; Saikia, Lakhinath published an article in Journal of Organic Chemistry. The title of the article was 《Copper-Catalyzed Direct Syntheses of Phenoxypyrimidines from Chloropyrimidines and Arylboronic Acids: A Cascade Avenue and Unconventional Substrate Pairs》.Reference of 4,6-Dichloropyrimidine The author mentioned the following in the article:

This synthetic methodol. for phenoxypyrimidines I (R = Ph, 2-methylphenyl, 3-nitrophenyl, etc.; R1 = H, Cl; X = N, CH;) and Et 4-[(4-hydroxyphenyl)amino]-2-(methylsulfanyl)pyrimidine-5-carboxylate that avoids the direct use of phenols or their salts was described. In contrast to the general trend of delivering Suzuki-Miyaura cross-coupling products in reactions between aryl or alky halides and arylboronic acids, the substrate pairs used herein (chloropyrimidines and arylboronic acids RB(OH)2) led to C-O bond formation under the reaction conditions. In total, 25 phenoxypyrimidines I and Et 2-(methylthio)-4-phenoxypyrimidine-5-carboxylate, 6-(4-aminophenoxy)-1,3-dimethylpyrimidine-2,4(1H,3H)-dione, 2-((6-methoxypyridin-3-yl)oxy)pyrimidine were successfully synthesized using the described protocol, 6 of which had a structural resemblance to etravirine such as N-methyl-N-(6-phenoxypyrimidin-4-yl)pyrimidin-2-amine. The results came from multiple reactions, including the reaction of 4,6-Dichloropyrimidine(cas: 1193-21-1Reference of 4,6-Dichloropyrimidine)

4,6-Dichloropyrimidine(cas: 1193-21-1) is a member of organic chlorides. Organic chloride content in crude oil can be detected through specialized laboratory analysis. Care and attention are essential while sampling and testing.Reference of 4,6-Dichloropyrimidine

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

《Design, synthesis, and pharmacological evaluation of 4- or 6-phenyl-pyrimidine derivatives as novel and selective Janus kinase 3 inhibitors》 was written by Shu, Lei; Chen, Chengjuan; Huan, Xueting; Huang, Hao; Wang, Manman; Zhang, Jianqiu; Yan, Yile; Liu, Jianming; Zhang, Tiantai; Zhang, Dayong. Application In Synthesis of 4,6-Dichloropyrimidine And the article was included in European Journal of Medicinal Chemistry in 2020. The article conveys some information:

In this work, poorly selective compounds based on 4- or 6-phenyl-pyrimidine derivatives I and II [R = H, prop-2-enamidyl, but-2-enamidyl, 2-cyanoacetamidyl; R1 = 1-methyl-1H-pyrazol-4-yl, 1-(2-methoxyethyl)-1H-pyrazol-4-yl, 4-(4-morpholinyl)phenyl, etc.; R2 = H, prop-2-enamidyl, but-2-enamidyl, 2-cyanoacetamidyl] have been improved to highly potent and selective compounds by designing a covalent binding tether, which attaches to the unique cysteine (Cys909) residue in JAK3. Compound II [R = prop-2-enamidyl; R1 = 4-(4-morpholinyl)phenyl, R2 = H (A)] exhibited potent JAK3 inhibitory activity (IC50 = 1.7 nM) with an excellent selectivity profile when compared to the other JAK isoforms (>588-fold). In a cellular assay, compound (A) strongly inhibited JAK3-dependent signaling and T cell proliferation. Moreover, in vivo data revealed that compound (A) significantly suppressed oxazolone (OXZ)-induced delayed hypersensitivity responses in Balb/c mice. Compound (A) also displayed decent pharmacokinetic properties and was suitable for in vivo use. Taken together, these results indicated that compound (A) may be a promising tool compound as a selective JAK3 inhibitor for treating autoimmune diseases. The experimental process involved the reaction of 4,6-Dichloropyrimidine(cas: 1193-21-1Application In Synthesis of 4,6-Dichloropyrimidine)

4,6-Dichloropyrimidine(cas: 1193-21-1) is a member of organic chlorides. Organic chloride content in crude oil can be detected through specialized laboratory analysis. Care and attention are essential while sampling and testing.Application In Synthesis of 4,6-Dichloropyrimidine

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

《Structure-Activity Relationship Study of Covalent Pan-phosphatidylinositol 5-Phosphate 4-Kinase Inhibitors》 was written by Manz, Theresa D.; Sivakumaren, Sindhu C.; Yasgar, Adam; Hall, Matthew D.; Davis, Mindy I.; Seo, Hyuk-Soo; Card, Joseph D.; Ficarro, Scott B.; Shim, Hyeseok; Marto, Jarrod A.; Dhe-Paganon, Sirano; Sasaki, Atsuo T.; Boxer, Matthew B.; Simeonov, Anton; Cantley, Lewis C.; Shen, Min; Zhang, Tinghu; Ferguson, Fleur M.; Gray, Nathanael S.. Recommanded Product: 1193-21-1 And the article was included in ACS Medicinal Chemistry Letters in 2020. The article conveys some information:

Phosphatidylinositol 5-phosphate 4-kinases (PI5P4Ks) are important mol. players in a variety of diseases, such as cancer. Currently available PI5P4K inhibitors are reversible small mols., which may lack selectivity and sufficient cellular on-target activity. In this study, we present a new class of covalent pan-PI5P4K inhibitors with potent biochem. and cellular activity. Our designs are based on THZ-P1-2, a covalent PI5P4K inhibitor previously developed in our laboratory Here, we report further structure-guided optimization and structure-activity relationship (SAR) study of this scaffold, resulting in compound 30(I), which retained biochem. and cellular potency, while demonstrating a significantly improved selectivity profile. Furthermore, we confirm that the inhibitors show efficient binding affinity in the context of HEK 293T cells using isothermal CETSA methods. Taken together, I represents a highly selective pan-PI5P4K covalent lead mol. In the experiment, the researchers used 4,6-Dichloropyrimidine(cas: 1193-21-1Recommanded Product: 1193-21-1)

4,6-Dichloropyrimidine(cas: 1193-21-1) is a member of organic chlorides. Organic chloride content in crude oil can be detected through specialized laboratory analysis. Care and attention are essential while sampling and testing.Recommanded Product: 1193-21-1

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

《Design, synthesis, and anticancer evaluation of acetamide and hydrazine analogues of pyrimidine》 was published in Journal of Heterocyclic Chemistry in 2020. These research results belong to Khazir, Jabeena; Mir, Bilal Ahmad; Chashoo, Gousia; Maqbool, Tariq; Riley, Darren; Pilcher, Lynne. Product Details of 1193-21-1 The article mentions the following:

A library of acetamide I [R = 2-hydroxyethylamino, 1-pyrrolidinyl, N-morpholinyl, etc.] and hydrazine II [R1 = 1-pyrrolidinyl, 1-piperidinyl, N-morpholinyl, 4-propanoyl-1-piperidyl; R2 = H, 2-Br, 3,4-di-MeO, etc.] analogs were generated on the pyrimidine ring through a multistep reaction starting from 5-nitro-pyrimidine-4,6-diol and pyrimidine-4,6-diol, resp. The synthesized analogs I and II were screened for in-vitro cytotoxic activity against various human cancer cell lines like HCT-1 and HT-15 (colon), MCF-7(breast), PC-3 (prostrate), SF268 (CNS) using MTT method. From the bioassay results, it was observed that even though many of the synthesized derivatives I and II exhibited a good potency against various screened cancer cell lines, compound I [R = 1-piperidinyl] showed potent anticancer activity on all the tested cancer cell lines with IC50 value of 0.36μM on CNS cell line and 1.6μM on HT-21 cell line, and compound II [R1 = N-morpholinyl, R2 = 2-OH] showed potent activity against three tested cancer cell lines with IC50 value of 0.76μM on HT-29 cell line, 2.6μM on HCT-15 and 3.2μM on MCF-7 cell line. After reading the article, we found that the author used 4,6-Dichloropyrimidine(cas: 1193-21-1Product Details of 1193-21-1)

4,6-Dichloropyrimidine(cas: 1193-21-1) is a member of organic chlorides. Almost all organochlorine compounds are synthesized. It is widely used as intermediates, solvents and pesticides of chemical synthetic products.Product Details of 1193-21-1

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

《Introducing rigid pyrimidine ring to improve the mechanical properties and thermal-oxidative stabilities of phthalonitrile resin》 was written by Yang, Kaixiong; Chen, Xinggang; Zhang, Zhenjiang; Yu, Xiaoyan; Naito, Kimiyoshi; Zhang, Qingxin. Formula: C4H2Cl2N2 And the article was included in Polymers for Advanced Technologies in 2020. The article conveys some information:

In this study, a novel phthalonitrile monomer containing pyrimidine ring, 4,6-bis[3-(3,4-dicyanophenoxy)phenoxy]pyrimidine (BCPM), was successfully synthesized by nucleophilic substitution reaction with resorcinol, 4,6-dichloropyrimidine and 4-nitrophthalonitrile. The BCPM monomer was cured by different temperature programs with 4-(aminophenoxy)phthalonitrile (APPH) as catalyst to give the polymers. The mol. structures of the BCPM monomer and the polymers were investigated by Fourier transform IR (FTIR) spectroscopy and NMR (NMR) spectroscopy. Differential scanning calorimetric (DSC) anal. was performed to study the processability of the BCPM monomer, which showed a wide processing window of about 117°. The mech. properties and thermal-oxidative stability of the polymer were characterized by dynamic mech. anal. (DMA) and thermogravimetric anal. (TGA), resp., which indicated that the polymers exhibited excellent storage modulus, high glass transition temperature over 400°, and outstanding thermal stability. The polymers also have low water absorption capacity and are suitable for humid environments. In the experiment, the researchers used 4,6-Dichloropyrimidine(cas: 1193-21-1Formula: C4H2Cl2N2)

4,6-Dichloropyrimidine(cas: 1193-21-1) is a member of organic chlorides. Organic chloride content in crude oil can be detected through specialized laboratory analysis. Care and attention are essential while sampling and testing.Formula: C4H2Cl2N2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

《Novel N-thioamide analogues of pyrazolylpyrimidine based piperazine: Design, synthesis, characterization, in-silico molecular docking study and biological evaluation》 was written by Vekariya, Mayur K.; Patel, Dhaval B.; Pandya, Pranav A.; Vekariya, Rajesh H.; Shah, Prapti U.; Rajani, Dhanji P.; Shah, Nisha K.. COA of Formula: C4H2Cl2N2This research focused onthioureidopiperazinyl pyrimidinyl pyrazolecarboxylate preparation antitubercular antimalaria antibacterial antifungal activity; structure thioureidopiperazinyl pyrimidinyl pyrazolecarboxylate antitubercular antimalaria antibacterial antifungal activity; mol docking thioureidopiperazinyl pyrimidinyl pyrazolecarboxylate DHFR FabH hydrolase; calculated hERG inhibition biol permeability thioureidopiperazinyl pyrimidinyl pyrazolecarboxylate; solubility polar surface area calculated thioureidopiperazinyl pyrimidinyl pyrazolecarboxylate. The article conveys some information:

(Thioureidopiperazinyl)pyrimidinyl pyrazolecarboxylates I (R = Ph, Me, Et, n-Pr, Bu, i-Pr, t-Bu, H2C:CHCH2, cyclohexyl, PhCH2, 2-MeOC6H4, 3-MeOC6H4, 4-MeOC6H4, 3-ClC6H4, 4-ClC6H4, 4-FC6H4, 2,4-Cl2C6H3, 3-IC6H4, 4-MeC6H4, PhCO, 4-O2NC6H4, 2,3-Cl2C6H3, 2,6-Cl2C6H3, 2-ClC6H4) were prepared and tested as potential antituberculosis, antimalarial, antibacterial, and antifungal agents. Their physicochem., biol. permeabilities into cells and through the blood-brain barrier, and hERG inhibition were calculated and the binding to Plasmodium falciparum dihydrofolate reductase, Escherichia coli FabH, and Staphylococcus aureus hydrolase were calculated for selected compounds In addition to this study using 4,6-Dichloropyrimidine, there are many other studies that have used 4,6-Dichloropyrimidine(cas: 1193-21-1COA of Formula: C4H2Cl2N2) was used in this study.

4,6-Dichloropyrimidine(cas: 1193-21-1) is a member of organic chlorides. Organic chlorides are compounds containing a carbon-chlorine bond, which are widely used in the oil field as a wax dissolver. They are generally not present in crude oils and are typically the result of additives, cleaning solutions or chemicals used for oil recovery.COA of Formula: C4H2Cl2N2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia